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Design, synthesis, and antiviral properties of 2-aryl-1H-benzimidazole-4-carboxamide derivatives

Xianjin LUO, Zhonglü ZHANG, Yutian YANG, Fei XUE, Naiyun XIU, Yuanbin SHE

《化学科学与工程前沿（英文）》 2009年 第3卷 第3期   页码 305-309 doi: 10.1007/s11705-009-0021-z

摘要： A series of new benzimidazole derivatives were designed and synthesized. Their chemical structures were testified by H NMR, infrared spectroscopy (IR), mass spectrography (MS), and elemental analysis. Their potent antiviral properties indicated the prospect of new drugs. Compound , , , , , , and were identified as novel antivirus with much better selective activity and inhibitory activity than the comparable ribavirin against Coxsackie virus B in VERO cells.

关键词： benzimidazole     coxsackie virus B3     antiviral properties    

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Direct acting antiviral-induced dynamic reduction of serum

Tung Huynh, Ke-Qin Hu

《医学前沿（英文）》 2019年 第13卷 第6期   页码 658-666 doi: 10.1007/s11684-019-0707-7

摘要： Direct acting antiviral (DAA) treatments may reduce the elevated α fetoprotein (AFP), but data on how these treatments affect elevated AFP in patients with chronic hepatitis C (CHC) remain insufficient. In the present study, the frequency of baseline AFP elevations and their related factors, AFP dynamics during and after DAA treatment, and factors associated with AFP reduction was assessed. This retrospective study included 141 patients with CHC without hepatocellular carcinoma who received DAA and achieved sustained virological response. The details are as follows: mean post-treatment follow-up was 99 weeks (12–213); mean age, 57.8 years old; 52%, males; 79%, genotype (GT) 1; and 47%, cirrhosis. Pre-treatment AFP elevation (>5.5 ng/mL) was seen in 48.2% patients. On multivariate analysis, baseline AFP>5.5 was associated with the presence of cirrhosis ( =0.001), co-existing non-alcoholic steatohepatitis (NASH) ( = 0.035), and GT 1 ( = 0.029). AFP normalization was seen in 28.2% patients at treatment week 2, in 52% at the end of treatment, and in 73.4% at the end of follow-up. Post-treatment week 24 AFP normalization was associated with the absence of cirrhosis ( = 0.003), Child–Pugh score<6 ( = 0.015), and baseline AFP<10 ( = 0.015). AFP elevation is common in patients with CHC and independently associated with NASH, cirrhosis, and GT 1. DAA treatment resulted in AFP normalization as early as treatment week 2. Post-treatment week 24 AFP normalization is independently associated with the absence of cirrhosis, Child–Pugh score<6, and baseline AFP<10.

关键词： chronic hepatitis C     α fetoprotein     direct acting antiviral treatment     cirrhosis    

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ROUTE DEVELOPMENT, ANTIVIRAL STUDIES, FIELD EVALUATION AND TOXICITY OF AN ANTIVIRAL PLANT PROTECTANT

《农业科学与工程前沿（英文）》 2022年 第9卷 第1期 doi: 10.15302/J-FASE- 2021390

摘要：

It has previously been shown that tryptophan, the biosynthesis precursor of Peganum harmala alkaloids, and its derivatives have anti-TMV activity both in vitro and in vivo. Further exploration of this led to the identification of NK0238 as a highly effective agent for the prevention and control of diseases caused by plant viruses, but the existing routes are unsuitable for its large-scale synthesis. This study optimized a route for two-step synthesis of this virucide candidate via reaction of l-tryptophan with triphosgene to produce l-tryptophan-N-carboxylic anhydride, which then reacts with n-octylamine to give NK0238 at up to 94% yield and nearly 97% HPLC purity. In addition, the route was used for the preparation of NK0238 on a>40 g scale permitting further assessment of its antivirus activity in the greenhouse and field experiments, and toxicity tests. NK0238 exhibited useful antiviral activities against a variety of viruses both in greenhouse and field experiments. The toxicity tests showed that NK0238 was not acutely toxic to birds, fish, honey bees and silkworms. The optimized route provides a solid foundation for its large-scale synthesis and subsequent efficacy and toxicity studies, its excellent activity and safety make NK0238 a promising drug candidate for further development.

 

关键词： antiviral plant protectant / antiviral in the greenhouse / field evaluation / l-trp-NCA / synthesis optimization / toxicity tests    

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ROUTE DEVELOPMENT, ANTIVIRAL STUDIES, FIELD EVALUATION AND TOXICITY OF AN ANTIVIRAL PLANT PROTECTANT

Wentao XU, Hao TIAN, Hongjian SONG, Yuxiu LIU, Yongqiang LI, Qingmin WANG

《农业科学与工程前沿（英文）》   页码 110-119 doi: 10.15302/J-FASE-2021390

摘要： It has previously been shown that tryptophan, the biosynthesis precursor of alkaloids, and its derivatives have anti-TMV activity both and . Further exploration of this led to the identification of NK0238 as a highly effective agent for the prevention and control of diseases caused by plant viruses, but the existing routes are unsuitable for its large-scale synthesis. This study optimized a route for two-step synthesis of this virucide candidate via reaction of L-tryptophan with triphosgene to produce L-tryptophan- -carboxylic anhydride, which then reacts with -octylamine to give NK0238 at up to 94% yield and nearly 97% HPLC purity. In addition, the route was used for the preparation of NK0238 on a > 40 g scale permitting further assessment of its antivirus activity in the greenhouse and field experiments, and toxicity tests. NK0238 exhibited useful antiviral activities against a variety of viruses both in greenhouse and field experiments. The toxicity tests showed that NK0238 was not acutely toxic to birds, fish, honey bees and silkworms. The optimized route provides a solid foundation for its large-scale synthesis and subsequent efficacy and toxicity studies, its excellent activity and safety make NK0238 a promising drug candidate for further development.

关键词： antiviral plant protectant     antiviral in the greenhouse     field evaluation     L-trp-NCA     synthesis optimization     toxicity tests    

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Critical roles of chemokines and cytokines in antiviral innate immune responses during rabies virus infection

Ying HUANG, Clement Wesley GNANADURAI, Zhenfang FU

《农业科学与工程前沿（英文）》 2017年 第4卷 第3期   页码 260-267 doi: 10.15302/J-FASE-2016116

摘要： The innate immune response is the first line of defense against viral invasion and pro-inflammatory chemokines and cytokines have a critical function in the innate immune responses against virus infections. The ability of a rabies virus (RABV) to induce the expression of chemokines and cytokines can lead to viral clearance from the central nervous system (CNS), whereas the ability to evade such expression and activation contributes to virulence and pathogenicity. In this review, the crucial contribution of chemokines/cytokines to clearing RABV from the CNS is discussed, including recruiting leukocytes into the CNS, enhancement of blood brain barrier permeability and activation of various immune cells that are essential for viral clearance. In addition, recombinant RABV expressing cytokines and chemokines can induce elevated innate and adaptive immune responses which result in clearing an established wild-type RABV infection in the CNS.

关键词： antiviral     blood brain barrier     chemokines and cytokines     innate immunity     rabies virus    

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ANTIVIRAL EFFECTS OF BACTERIOCIN AGAINST ANIMAL-TO-HUMAN TRANSMITTABLE MUTATED SARS-COV-2: A SYSTEMATIC

《农业科学与工程前沿（英文）》 2021年 第8卷 第4期   页码 603-622 doi: 10.15302/J-FASE -2021397

摘要：

The COVID-19 infections caused by SARS-CoV-2 have resulted in millions of people being infected and thousands of deaths globally since November 2019. To date, no unique therapeutic agent has been developed to slow the progression of this pandemic. Despite possessing antiviral traits the potential of bacteriocins to combat SARS-CoV-2 infection has not been fully investigated. This review summarizes the mechanisms by which bacteriocins can be manipulated and implemented as effective virus entry blockers with infection suppression potential properties to highly transmissible viruses through comprehensive immune modulations that are potentially effective against COVID-19. These antimicrobial peptides have been suggested as effective antiviral therapeutics and therapeutic supplements to prevent rapid virus transmission. This review also provides a new insight into the cellular and molecular alterations which have made SARS-CoV-2 self-modified with diversified infection patterns. In addition, the possible applications of antimicrobial peptides through both natural and induced mechanisms in infection prevention perspectives on changeable virulence cases are comprehensively analyzed. Specific attention is given to the antiviral mechanisms of the molecules along with their integrative use with synthetic biology and nanosensor technology for rapid detection. Novel bacteriocin based therapeutics with cutting-edge technologies might be potential substitutes for existing time-consuming and expensive approaches to fight this newly emerged global threat.

 

关键词： antimicrobial proteins / antiviral profiling of bacteriocins / antiviral therapeutics / immunomodulation / nanosensor technology / mutated SARS-CoV-2    

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Current recommendations of managing HBV infection in preconception or pregnancy

null

《医学前沿（英文）》 2014年 第8卷 第2期   页码 158-165 doi: 10.1007/s11684-014-0340-4

摘要：

Hepatitis B remains a leading cause of cirrhosis, hepatocellular carcinoma and liver transplantation worldwide. Management of chronic hepatitis B during pregnancy is challenging. Transmission of hepatitis B to infants still occurs perinatally although immunoprophylaxis is widely available for infants born to mothers with chronic hepatitis B infection. The emerging data suggest that initiation of antiviral therapy in the beginning of the third trimester in highly viremic mothers can prevent immunoprophylaxis failure in their infants. The available drug safety data show that lamivudine, telbivudine and tenofovir are generally safe to be used during the pregnancy. In order to minimize the fetal exposure to the antiviral medication, antiviral therapy during the pregnancy should be limited to a selected group of patients with cirrhosis, high hepatitis B viral load, or prior history immunoprophylaxis failure. An elective Caesarean section may reduce the risk of perinatal transmission. For those females planning for pregnancy or in early stage of pregnancy, communication and follow-up among obstetrician, gastroenterologist, and primary care physician are important. In this article, we will review the features of hepatitis B infection before, during and after the pregnancy; the risk factors that increase mother-to-child transmission; safety data on antiviral drug use during pregnancy; and the potential role of Caesarean section in selected cases.

关键词： antiviral therapy     Caesarean section     cirrhosis     hepatitis B     immunoprophylaxis     mother-to-child transmission     pregnancy     prevention    

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Oral administration of

Sufen ZHAO,Yuanyuan JIA,Weiwei ZHANG,Lili WANG,Yunfei MA,Kedao TENG

《农业科学与工程前沿（英文）》 2015年 第2卷 第4期   页码 318-326 doi: 10.15302/J-FASE-2015080

摘要： Garlic ( Liliaceae) has been safely used for more than 5000 years, and research on garlic extract is rapidly increasing because of its multiple biological functions. The effects of oral administration of garlic mixture (GM, water-soluble extract) on infectious bursal disease virus (IBDV)-infected specific pathogen free male white leghorn chicken were examined through histopathological, immunohistochemical, and Western blot analyses, and enzyme-linked immunosorbent assay. The results confirmed the protective effects of oral administration of 5 mg·kg BW GM (Group GM1) on bursal lesions after IBDV infection. In particular, protein expression of IBDV in the bursa decreased in Group GM1, indicating that GM administration decreased IBDV replication in the bursa. Furthermore, immunoglobulin M- and A-bearing B lymphocytes significantly increased 7 days post infection in bursae in Group GM1 ( <0.01), suggesting that the oral administration of 5 mg·kg GM offers moderate protection against B cell destruction after IBDV infection. During infection, the concentration of bursal interferon gamma (IFN-g) increased and peaked in Group GM1 earlier than in Group T (IBDV-exposed), demonstrating that GM administration prompted the production of IFN-g to protect against IBDV infection.

关键词： garlic     infectious bursal disease virus (IBDV)     antiviral effect     IgM-bearing B lymphocyte    

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A brief review of microRNA and its role in PRRSV infection and replication

Xuekun GUO,Wenhai FENG

《农业科学与工程前沿（英文）》 2014年 第1卷 第2期   页码 114-120 doi: 10.15302/J-FASE-2014022

摘要： Porcine reproductive and respiratory syndrome virus (PRRSV), a single-stranded RNA virus, mainly infects cells of monocyte/macrophage lineage. Recently, host microRNAs were shown to be capable of modulating PRRSV infection and replication by multiple ways such as targeting viral genomic RNA, targeting viral receptor and inducing antiviral response. MicroRNAs are small RNAs and have emerged as important regulators of virus-host cell interactions. In this review, we discuss the identified functions of host microRNAs in relation to PRRSV infection and propose that cellular microRNAs may have a substantial effect on cell or tissue tropism of PRRSV.

关键词： porcine reproductive and respiratory syndrome virus (PRRSV)     microRNA     antiviral     viral tropism    

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Potential use of serum HBV RNA in antiviral therapy for chronic hepatitis B in the era of nucleos(t)ide

null

《医学前沿（英文）》 2017年 第11卷 第4期   页码 502-508 doi: 10.1007/s11684-017-0590-z

摘要：

Although the efficacy of nucleos(t)ide analogue (NA) has been confirmed for treatment of chronic hepatitis B, long-term therapy has been recommended due to the high frequency of off-therapy viral DNA rebound and disease relapse. In this review, the RNA virion-like particles of hepatitis B virus (HBV) are integrated into the life cycle of HBV replication, and the potential significance of serum HBV RNA is systematically described. The production of HBV RNA virion-like particles should not be blocked by NA; in this regard, serum HBV RNA is found to be a suitable surrogate marker for the activity of intrahepatic covalently closed circular DNA (cccDNA), particularly among patients receiving NA therapy. Therefore, the concept of virological response is redefined as persistent loss of serum HBV DNA and HBV RNA. In contrast to hepatitis B surface antigen (HBsAg) that can originate from either the cccDNA or the integrated HBV DNA fragment, serum HBV RNA, with pregenomic RNA origination, can only be transcribed from cccDNA. Therefore, the loss of serum HBV RNA would likely be a promising predicator for safe drug discontinuation. The clinical status of consistent loss of serum HBV RNA accompanied with low serum HBsAg levels might be implicated as a “para-functional cure,” a status nearly close to the functional cure of chronic hepatitis B, to distinguish the “functional cure” characterized as serum HBsAg loss with or without anti-HBs seroconversion.

关键词： chronic hepatitis B     serum HBV RNA     nucleos(t)ide analogs     virological response     para-functional cure    

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Effect of different high viscosity modifiers on rheological properties of high viscosity asphalt

《结构与土木工程前沿（英文）》 2021年 第15卷 第6期   页码 1390-1399 doi: 10.1007/s11709-021-0775-z

摘要： High viscosity asphalt (HVA) has been a great success as a drainage pavement material. However, the larger porosity of drainage asphalt mixtures weakens the cohesion and adhesion and leads to premature rutting, water damage, spalling and cracking. The purpose of this study was to investigate the rheological properties of HVA prepared using different high viscosity modifiers through conventional tests, Brookfield viscosity tests, dynamic shear rheometer tests and bending beam rheometer tests. The conventional performance results demonstrated SBS + rubber asphalt (SRA-1/2) exhibited excellent elastic recovery and low-temperature flexibility. The 60°C dynamic viscosity results indicated TPS + rubber asphalt (TRA) had the excellent adhesion. The rotational viscosity results and rheological results indicated that SRA-2 not only exhibited excellent temperature stability and workability, as well as excellent resistance to deformation and rutting resistance, but also exhibited excellent low-temperature cracking resistance and relaxation performance. Based on rheological results, the PG classification of HVA was 16% rubber + asphalt for PG76-22, 20% rubber + asphalt for PG88-22, TRA and SRA-1/2 for PG88-28. From comprehensive evaluation of the viscosity, temperature stability and sensitivity, as well as high/low temperature performance of HVA, SRA-2 was found to be more suited to the requirements of drainage asphalt pavement materials.

关键词： high viscosity asphalt     rheological properties     rubber     modifier     viscosity    

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LINKING CROP WATER PRODUCTIVITY TO SOIL PHYSICAL, CHEMICAL AND MICROBIAL PROPERTIES

《农业科学与工程前沿（英文）》 2021年 第8卷 第4期   页码 545-558 doi: 10.15302/J-FASE -2020349

摘要：

Agriculture uses a large proportion of global and regional water resources. Due to the rapid increase of population in the world, the increasing competition for water resources has led to an urgent need in increasing crop water productivity for agricultural sustainability. As the medium for crop growth, soils and their properties are important in affecting crop water productivity. This review examines the effects of soil physical, chemical, and microbial properties on crop water productivity and the quantitative relationships between them. A comprehensive view of these relationships may provide important insights for soil and water management in arable land for agriculture in the future.

 

关键词： crop water productivity     crop yield     soil chemical properties     soil microbial properties     soil physical properties     water consumption    

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Effect of earth reinforcement, soil properties and wall properties on bridge MSE walls

《结构与土木工程前沿（英文）》 2021年 第15卷 第5期   页码 1209-1221 doi: 10.1007/s11709-021-0764-2

摘要： Mechanically stabilized earth (MSE) retaining walls are popular for highway bridge structures. They have precast concrete panels attached to earth reinforcement. The panels are designed to have some lateral movement. However, in some cases, excessive movement and even complete dislocation of the panels have been observed. In this study, 3-D numerical modeling involving an existing MSE wall was undertaken to investigate various wall parameters. The effects of pore pressure, soil cohesion, earth reinforcement type and length, breakage/slippage of reinforcement and concrete strength, were examined. Results showed that the wall movement is affected by soil pore pressure and reinforcement integrity and length, and unaffected by concrete strength. Soil cohesion has a minor effect, while the movement increased by 13–20 mm for flexible geogrid reinforced walls compared with the steel grid walls. The steel grid stresses were below yielding, while the geogrid experienced significant stresses without rupture. Geogrid reinforcement may be used taking account of slippage resistance and wall movement. If steel grid is used, non-cohesive soil is recommended to minimize corrosion. Proper soil drainage is important for control of pore pressure.

关键词： mechanically stabilized earth walls     precast concrete panels     backfill soil     finite element modeling     earth reinforcement    

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Mechanical properties and microstructure of multilayer graphene oxide cement mortar

《结构与土木工程前沿（英文）》 2021年 第15卷 第4期   页码 1058-1070 doi: 10.1007/s11709-021-0747-3

摘要： This study reports on the effects of multilayer graphene oxide (MGO) on compressive strength, flexural strength, and microstructure of cement mortar. The cement mortar was prepared with type P. II. 52.5 Portland cement, standard sand, and MGO. Four mixes were prepared with inclusion of MGO (0%, 0.02%, 0.04%, and 0.06% by weight of cement). The testing result shows that the compressive of GO-cement mortar increased by 4.84%–13.42%, and the flexural strength increased by 4.37%–8.28% at 3 d. GO-cement mortar’s compressive strength and flexural strength at 7 d increased by 3.84%–12.08% and 2.54%–13.43%, respectively. MGO made little contribution to the increases of compressive strength and flexural strength of cement mortar at 28 d. The results of X-ray diffraction (XRD), scanning electron microscope (SEM), and nitrogen (N2) adsorption/desorption tests show that the types of hydration products and crystal grain size did not change after adding MGO. Still, it can help to improve the microstructure of the cement mortar via regulating hydration products and can provide more condensed cores to accelerate hydration. Furthermore, the regulating action of MGO for the microstructure of cement mortar at an early age was better than that at 28 d.

关键词： graphene oxide     cement     mortar     mechanical properties     microstructure    

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Synthesis, characterization and assessment thermal properties of clay based nanopigments

Mohammad Banimahd KIEVANI, Milad EDRAKI

《化学科学与工程前沿（英文）》 2015年 第9卷 第1期   页码 40-45 doi: 10.1007/s11705-015-1505-7

摘要： Nano-clay based pigments (NCP) are new type of pigments composed of organic dyes and layered silicate-clay nano-particles, and have already been used in polymeric coatings to improve mechanical thermal and stability properties. In this paper, the basic blue 41(BB41) was intercalated into Na - montmorillonite in an aqueous medium. The dye-intercalated montmorillonite was centrifuged, dried, and milled to prepare the nanopigment particles. X-ray diffraction showed an increase in the basal spacing, thus confirming intercalation of the BB41 molecules within the nanostructures of the interlayer spaces. Fourier transform infrared spectroscopy was used for identifying the functional groups and chemical bounding of Na -montmorillonite, BB41 and montmorillonite-BB41. The morphology of NCP was also studied by transmission electron microscopy. Finally, thermo-gravimetric analysis and differential thermograms suggested the thermal stability of the intercalated dye was improved.

关键词： nanopigment     layered silicate     cationic dye     thermal properties    

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标题 作者 时间 类型 操作

Design, synthesis, and antiviral properties of 2-aryl-1H-benzimidazole-4-carboxamide derivatives

Xianjin LUO, Zhonglü ZHANG, Yutian YANG, Fei XUE, Naiyun XIU, Yuanbin SHE

期刊论文

Direct acting antiviral-induced dynamic reduction of serum

Tung Huynh, Ke-Qin Hu

期刊论文

ROUTE DEVELOPMENT, ANTIVIRAL STUDIES, FIELD EVALUATION AND TOXICITY OF AN ANTIVIRAL PLANT PROTECTANT

期刊论文

ROUTE DEVELOPMENT, ANTIVIRAL STUDIES, FIELD EVALUATION AND TOXICITY OF AN ANTIVIRAL PLANT PROTECTANT

Wentao XU, Hao TIAN, Hongjian SONG, Yuxiu LIU, Yongqiang LI, Qingmin WANG

期刊论文

Critical roles of chemokines and cytokines in antiviral innate immune responses during rabies virus infection

Ying HUANG, Clement Wesley GNANADURAI, Zhenfang FU

期刊论文

ANTIVIRAL EFFECTS OF BACTERIOCIN AGAINST ANIMAL-TO-HUMAN TRANSMITTABLE MUTATED SARS-COV-2: A SYSTEMATIC

期刊论文

Current recommendations of managing HBV infection in preconception or pregnancy

null

期刊论文

Oral administration of

Sufen ZHAO,Yuanyuan JIA,Weiwei ZHANG,Lili WANG,Yunfei MA,Kedao TENG

期刊论文

A brief review of microRNA and its role in PRRSV infection and replication

Xuekun GUO,Wenhai FENG

期刊论文

Potential use of serum HBV RNA in antiviral therapy for chronic hepatitis B in the era of nucleos(t)ide

null

期刊论文

Effect of different high viscosity modifiers on rheological properties of high viscosity asphalt

期刊论文

LINKING CROP WATER PRODUCTIVITY TO SOIL PHYSICAL, CHEMICAL AND MICROBIAL PROPERTIES

期刊论文

Effect of earth reinforcement, soil properties and wall properties on bridge MSE walls

期刊论文

Mechanical properties and microstructure of multilayer graphene oxide cement mortar

期刊论文

Synthesis, characterization and assessment thermal properties of clay based nanopigments

Mohammad Banimahd KIEVANI, Milad EDRAKI

期刊论文